首页> 外文OA文献 >In Vitro Activities of the Ketolides Telithromycin (HMR 3647) and HMR 3004 Compared to Those of Clarithromycin against Slowly Growing Mycobacteria at pHs 6.8 and 7.4
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In Vitro Activities of the Ketolides Telithromycin (HMR 3647) and HMR 3004 Compared to Those of Clarithromycin against Slowly Growing Mycobacteria at pHs 6.8 and 7.4

机译:在pH值为6.8和7.4时,酮碘化物Telithromycin(HMR 3647)和HMR 3004与克拉霉素的体外活性对缓慢增长的分枝杆菌的体外活性比较

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摘要

The in vitro activities of HMR 3647 (telithromycin) and HMR 3004, two novel semisynthetic ketolides, were investigated and compared with that of the reference macrolide drug, clarithromycin, against 34 strains of slowly growing mycobacteria at pHs 6.8 and 7.4, as determined radiometrically. The MICs at pH 7.4 were about 1 to 2 dilutions lower than those observed at pH 6.8. In terms of the highest to the lowest activity, the three antibiotics could be classified as follows: clarithromycin > HMR 3004 > HMR 3647. Among the species tested, Mycobacterium bovis BCG, M. ulcerans, M. avium, and M. paratuberculosis were moderately susceptible to HMR 3004 and HMR 3647 (MICs at pH 7.4, ≤5.0 and ≤20.0 μg/ml, respectively, versus ≤1.25 μg/ml for clarithromycin), whereas M. tuberculosis, M. africanum, M. bovis, and M. simiae were resistant (MICs, ≥10.0 and ≥40.0 μg/ml, respectively, at pH 7.4). Although not more active than clarithromycin in vitro, the high level of intracellular accumulation of the two ketolides inside phagocytes warrants further screening in experimental animal models.
机译:研究了HMR 3647(泰利霉素)和HMR 3004(两种新型的半合成酮醇)的体外活性,并将其与参考大环内酯类药物克拉霉素对34株缓慢生长的分枝杆菌在pH 6.8和7.4下的放射活性进行了比较,如放射线测定的。 pH 7.4时的MIC比pH 6.8时的MIC低约1-2倍。从最高活性到最低活性,可以将三种抗生素分类为:克拉霉素> HMR 3004> HMR3647。在所测试的物种中,牛分枝杆菌BCG,溃疡分枝杆菌,鸟分枝杆菌和副结核分枝杆菌中等。易受HMR 3004和HMR 3647影响(MIC分别为pH 7.4,≤5.0和≤20.0μg/ ml,克拉霉素为≤1.25μg/ ml),而结核分枝杆菌,非洲分枝杆菌,牛分枝杆菌和M. simiae具有抗性(在pH 7.4时,MIC分别≥10.0和≥40.0μg/ ml)。尽管在体外不比克拉霉素更具活性,但吞噬细胞内两种酮类化合物的高细胞内蓄积水平仍需要在实验动物模型中进行进一步筛选。

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